- Preparation method of N-methyltyramine hydrochloride
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The invention discloses a preparation method of N-methyltyramine hydrochloride. The method comprises the following steps: carrying out amination reaction on 4-(2-bromoethyl) phenol and a proper excess amount of monomethylamine according to a molar ratio of 4-(2-bromoethyl) phenol to monomethylamine of 1: (10-30) mol; meanwhile, a solvation effect is exerted, and a large amount of dilution is realized, so that the contact reaction opportunity of a generated product and 4-(2-bromoethyl)phenol which is added later is greatly reduced; and the high product yield can be kept, and meanwhile the low preparation cost is achieved. The invention further provides two simple and convenient recycling methods. Waste discharge can be greatly reduced, economic benefits of the preparation process are improved, and meanwhile a good environment protection effect is achieved.
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Paragraph 0039; 0050-0061
(2021/11/26)
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- Catalytic Strategy for Regioselective Arylethylamine Synthesis
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A mild, modular, and practical catalytic system for the synthesis of the highly privileged phenethylamine pharmacophore is reported. Using a unique combination of organic catalysts to promote the transfer of electrons and hydrogen atoms, this system performs direct hydroarylation of vinyl amine derivatives with a wide range of aryl halides (including aryl chlorides). This general and highly chemoselective protocol delivers a broad range of arylethylamine products with complete regiocontrol. The utility of this process is highlighted by its scalability and the modular synthesis of an array of bioactive small molecules.
- Boyington, Allyson J.,Seath, Ciaran P.,Zearfoss, Avery M.,Xu, Zihao,Jui, Nathan T.
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supporting information
p. 4147 - 4153
(2019/03/07)
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- Synthesis method of N-methyltyramine hydrochloride
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The invention relates to a synthesis method of N-methyltyramine hydrochloride and belongs to the technical field of organic synthesis. The synthesis method comprises dissolving p-hydroxyphenylacetic acid in a solvent 1, adding thionyl chloride into the solution, carrying out reflux stirring for a complete reaction, cooling the product, adding the reaction solution into an aqueous solution of methylamine drop by drop, then carrying out thermal insulation stirring, filtering the mixture to obtain an intermediate, dissolving the intermediate in a solvent 2, adding a reducer into the solution at the room temperature, then adding Lewis acid into the solution in batches, carrying out heating reflux stirring overnight, after the reaction is finished, introducing the reaction solution into an acid solution, adjusting pH to 7, stirring the solution, carrying out filtration and liquid separation, feeding hydrogen chloride gas into the second layer of the solvent until the hydrogen chloride gas is saturated and pH of the solution is 1, carrying out stirring and then pumping filtration, and carrying out solid leaching and drying to obtain N-methyltyramine hydrochloride. The synthesis method has the advantages of mild reaction conditions, high conversion rate, cheap and easily available raw materials, use of cheap conventional reagents, low synthesis cost, simple and easy post-treatment, no generation of a large amount of three wastes, high product yield, high purity and good quality.
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Paragraph 0028; 0030; 0031; 0033; 0034; 0036; 0037; 0039
(2017/08/29)
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- Total synthesis and biological evaluation of methylgerambullone
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First total synthesis of methylgerambullone (MGB, 1) isolated from Glycosmis angustifolia was completed via a convergent route. The effect of MGB on the contractile responses of the isolated guinea-pig ileum induced by acetylcholine was investigated. As a result, it showed a potent relaxation rate (78.66 ± 4.30% at 100 mg/L) in a concentration-dependent manner on longitudinal smooth muscle contraction of isolated guinea-pig ileum induced by 1 μM acetylcholine.
- Moon, Jong Taik,Ha, Sung Hoon,Lee, So Hyung,Kwon, Tae Hui,Oh, Chun Rim,Kim, Young Deuk,Kim, Jungahn,Choo, Dong Joon,Lee, Jae Yeol
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scheme or table
p. 52 - 55
(2010/04/24)
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